Abstract: Intestinal Peyer's patches (PPs) are important sites to induce mucosal immunity response. As a kind of specialized epithelial cells in PPs, microfold cells (M cells) have a unique ability to take up antigens and can promote systemic immune response by transferring antigens to dendritic cells (DCs) in PPs. Selecting a suitable drug delivery vehicle and modifying the vehicle with a specific ligand can target drugs and bioactive substances to M cells to exert a therapeutic effect on intestinal immune-related diseases. This paper reviews the relevant literatures in the past 20 years, and summarizes and analyzes the ligands, types of vehicles, material properties that target M cells and main factors affecting the uptake of M cells, in order to provide construction ideas and experimental methods that can be worthy of reference for the study of PPs M cells-targeting drug delivery strategies.